JP6373275B2 - 肺動脈高血圧症及び肺障害の治療に使用するための1,3‐ジヒドロイミダゾール‐2‐チオン誘導体 - Google Patents
肺動脈高血圧症及び肺障害の治療に使用するための1,3‐ジヒドロイミダゾール‐2‐チオン誘導体 Download PDFInfo
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- JP6373275B2 JP6373275B2 JP2015542997A JP2015542997A JP6373275B2 JP 6373275 B2 JP6373275 B2 JP 6373275B2 JP 2015542997 A JP2015542997 A JP 2015542997A JP 2015542997 A JP2015542997 A JP 2015542997A JP 6373275 B2 JP6373275 B2 JP 6373275B2
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- thione
- dihydroimidazol
- aminoethyl
- compound
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- 238000011282 treatment Methods 0.000 title claims description 42
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 title claims description 40
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- 208000019693 Lung disease Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims description 131
- 229960003065 bosentan Drugs 0.000 claims description 37
- ZSSLCFLHEFXANG-GOSISDBHSA-N 4-[2-(benzylamino)ethyl]-3-[(3r)-6,8-difluoro-3,4-dihydro-2h-chromen-3-yl]-1h-imidazole-2-thione Chemical compound C=1NC(=S)N([C@H]2COC3=C(F)C=C(C=C3C2)F)C=1CCNCC1=CC=CC=C1 ZSSLCFLHEFXANG-GOSISDBHSA-N 0.000 claims description 34
- 150000003839 salts Chemical class 0.000 claims description 34
- -1 hydroxy, nitro, amino Chemical group 0.000 claims description 32
- 239000008194 pharmaceutical composition Substances 0.000 claims description 29
- 239000008186 active pharmaceutical agent Substances 0.000 claims description 20
- CWWWTTYMUOYSQA-LLVKDONJSA-N 4-(2-aminoethyl)-3-[(3r)-6,8-difluoro-3,4-dihydro-2h-chromen-3-yl]-1h-imidazole-2-thione Chemical compound NCCC1=CNC(=S)N1[C@@H]1CC2=CC(F)=CC(F)=C2OC1 CWWWTTYMUOYSQA-LLVKDONJSA-N 0.000 claims description 19
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- 206010013975 Dyspnoeas Diseases 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 239000001257 hydrogen Substances 0.000 claims description 14
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- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 150000002367 halogens Chemical class 0.000 claims description 10
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- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical class N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims description 7
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- Vascular Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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US201261726119P | 2012-11-14 | 2012-11-14 | |
US61/726,119 | 2012-11-14 | ||
PCT/PT2013/000065 WO2014077715A1 (en) | 2012-11-14 | 2013-11-14 | 1,3-dihydroimidazole-2-thione derivatives for use in the treatment of pulmonary arterial hypertension and lung injury |
Publications (3)
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JP2016504286A JP2016504286A (ja) | 2016-02-12 |
JP2016504286A5 JP2016504286A5 (sr) | 2017-01-12 |
JP6373275B2 true JP6373275B2 (ja) | 2018-08-15 |
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JP2015542997A Expired - Fee Related JP6373275B2 (ja) | 2012-11-14 | 2013-11-14 | 肺動脈高血圧症及び肺障害の治療に使用するための1,3‐ジヒドロイミダゾール‐2‐チオン誘導体 |
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US (3) | US9604970B2 (sr) |
EP (1) | EP2919780B1 (sr) |
JP (1) | JP6373275B2 (sr) |
KR (1) | KR102259938B1 (sr) |
CN (1) | CN105025895B (sr) |
AU (1) | AU2013345494B2 (sr) |
BR (1) | BR112015010969B1 (sr) |
CA (1) | CA2890920C (sr) |
CY (1) | CY1120953T1 (sr) |
DK (1) | DK2919780T3 (sr) |
ES (1) | ES2693025T3 (sr) |
HK (1) | HK1215393A1 (sr) |
HR (1) | HRP20181651T1 (sr) |
IN (1) | IN2015DN04089A (sr) |
LT (1) | LT2919780T (sr) |
MX (1) | MX355422B (sr) |
PL (1) | PL2919780T3 (sr) |
PT (1) | PT2919780T (sr) |
RS (1) | RS57874B1 (sr) |
RU (1) | RU2718055C2 (sr) |
SI (1) | SI2919780T1 (sr) |
TR (1) | TR201815850T4 (sr) |
WO (1) | WO2014077715A1 (sr) |
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ES2693025T3 (es) | 2012-11-14 | 2018-12-07 | Bial - Portela & Ca., S.A. | Derivados de 1,3-dihidroimidazol-2-tiona para su uso en el tratamiento de hipertensión arterial pulmonar y lesión pulmonar |
GB201810395D0 (en) * | 2018-06-25 | 2018-08-08 | Bial Portela & Ca Sa | Formulations comprising dopamine-beta-hydroxylase inhibitors and methods for their preparation |
WO2021005623A1 (en) * | 2019-07-08 | 2021-01-14 | Msd Wellcome Trust Hilleman Laboratories Pvt. Ltd. | A vaccine formulation for protection against enterotoxigenic e. coli (etec) and cholera |
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JPH0623107B2 (ja) * | 1990-11-16 | 1994-03-30 | 帝人株式会社 | プロスタサイクリン類を有効成分とする薬学的組成物 |
ATE243199T1 (de) * | 1994-04-26 | 2003-07-15 | Syntex Llc | Benzocyclohexylimidazolthion-derivate |
TW536540B (en) | 1997-01-30 | 2003-06-11 | Bristol Myers Squibb Co | Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe |
US7125904B2 (en) * | 2002-10-11 | 2006-10-24 | Portela & C.A., S.A. | Peripherally-selective inhibitors of dopamine-β-hydroxylase and method of their preparation |
US20040102361A1 (en) * | 2002-11-27 | 2004-05-27 | Frederic Bodin | Pharmaceutical composition for the treatment of pulmonary arterial hypertension |
GB0600709D0 (en) | 2006-01-13 | 2006-02-22 | Portela & Ca Sa | Drug combinations |
GB0610804D0 (en) * | 2006-05-31 | 2006-07-12 | Portela & Ca Sa | New crystal forms |
GB0700635D0 (en) | 2007-01-12 | 2007-02-21 | Portela & Ca Sa | Therapy |
EP2146707A2 (en) * | 2007-05-03 | 2010-01-27 | Abraxis BioScience, LLC | Methods and compositions for treating pulmonary hypertension |
GB0708818D0 (en) * | 2007-05-08 | 2007-06-13 | Portela & Ca Sa | Compounds |
WO2009072915A1 (en) * | 2007-12-05 | 2009-06-11 | Bial - Portela & Ca., S.A. | New salts and crystal forms |
BRPI0821970A2 (pt) | 2008-01-03 | 2015-06-23 | Biomarin Pharm Inc | Análogos de pterina para tratamento de condição responsiva a bh4 |
AR070841A1 (es) * | 2008-03-13 | 2010-05-05 | Bial Portela & Ca Sa | Proceso de hidrogenacion catalitica asimetrica |
AR071632A1 (es) * | 2008-05-06 | 2010-06-30 | Bial Portela & Ca Sa | Proceso catalitico para hidrogenacion asimetrica en la sintesis de inhibidores de la dopamina-beta-hidroxilasa" |
DE102008054205A1 (de) * | 2008-10-31 | 2010-05-06 | Bayer Schering Pharma Aktiengesellschaft | Verwendung von Helium-Sauerstoff-Gasgemischen zur Behandlung der pulmonalen arteriellen Hypertonie |
JP6161538B2 (ja) * | 2010-12-22 | 2017-07-12 | バイアル−ポルテラ アンド シーエー,エス.エー. | 結晶形及びその製造方法 |
ES2693025T3 (es) | 2012-11-14 | 2018-12-07 | Bial - Portela & Ca., S.A. | Derivados de 1,3-dihidroimidazol-2-tiona para su uso en el tratamiento de hipertensión arterial pulmonar y lesión pulmonar |
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2016
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